ANTI MALARIALS CHAP 7

Question 1

How is malaria transmitted to humans?

Answer 1

By the Anopheles mosquito

Question 2

What parasite causes malaria?

Answer 2

Plasmodium parasite

Question 3

Which Plasmodium species causes the most severe form of malaria?

Answer 3

Plasmodium falciparum

Question 4

What percentage of erythrocytes can Plasmodium falciparum infect?

Answer 4

Up to 65%

Question 5

Which is the second most common species of Plasmodium?

Answer 5

Plasmodium vivax

Question 6

Why is Plasmodium vivax known for recurrence?

Answer 6

It can reinfect liver cells

Question 7

Which Plasmodium species causes about 10% of malarial cases and frequent relapses?

Answer 7

Plasmodium malariae

Question 8

What is the least common Plasmodium species?

Answer 8

Plasmodium ovale

Question 9

What does the word ‘malaria’ mean?

Answer 9

“Mala aria” or bad air

Question 10

What are other names historically given to malaria?

Answer 10

-Ague
-intermittent fever
-marsh fever
-The Fever

Question 11

When is the Anopheles mosquito active?

Answer 11

At night (nocturnal feeder)

Question 12

How can the Anopheles mosquito be eliminated?

Answer 12

By using insecticides such as DDT (Dichlorodiphenyltrichloroethane).

Question 13

Name six human mutations that offer protection against malaria.

Answer 13

-Sickling disease (sickle cell anemia)

-G6PD deficiency

-Hemoglobin C

-Thalassemia

-Increased nitric oxide (NO) production

-Pyruvate kinase deficiency

Question 14

List the four targets for antimalarial drugs.

Answer 14

-Kill sporozoites/prevent liver entry

-Kill schizonts in hepatocytes/prevent merozoite formation

-Kill merozoites in blood/prevent gametocyte development

-Kill gametocytes before mosquito uptake

Question 15

What structural feature is common in antimalarial drugs?

Answer 15

A quinoline ring or an acridine ring (quinoline with an additional benzene).

Question 16

From which plant are cinchona alkaloids derived?

Answer 16

Cinchona succirubra and Cinchona calisaya

Question 17

What key structure is present in cinchona alkaloids?

Answer 17

A quinuclidine ring

Question 18

For what malaria strain is quinine reserved?

Answer 18

Chloroquine-resistant P. falciparum

Question 19

Aside from malaria, what else is quinine used for?

Answer 19

Nocturnal leg cramps

Question 20

What is quinine’s pregnancy category?

Answer 20

Category X (abortifacient)

Question 21

What is the MOA of quinine?

Answer 21

Inhibits nucleic acid synthesis, protein synthesis, glycolysis in P. falciparum, and binds with hemazoin in erythrocytes.

Question 22

Is quinidine used for malaria?

Answer 22

No, but it’s a more potent and more toxic agent than quinine.

Question 23

What is the primary use of quinidine?

Answer 23

Treating cardiac arrhythmias

Question 24

What syndrome is associated with quinine toxicity?

Answer 24

Cinchonism

Question 25

List symptoms of cinchonism.

Answer 25

Nausea, vomiting, tinnitus, vertigo, GI issues, nervous system effects, cardiovascular effects, and skin reactions.

Question 26

* closest antimalarials that are bases on quinine structure * substituted at the same position 4 as quinine and have assymetric carbon equivalent to quinine's C9 position

Answer 26

7-Chloro-4-Aminoquinolines

Question 27

At what position are substitutions made in 7-Chloro-4-Aminoquinolines?

Answer 27

Position 4

Question 28

What antimalarial is most similar to quinine structurally?

Answer 28

Chloroquine

Question 29

What is the DOC for erythrocytic P. falciparum malaria and used for both prophylaxis and treatmant of P. ovale, P. vivax and P. malariae infections?

Answer 29

Chloroquine

Question 30

Is chloroquine effective against exoerythrocytic parasites?

Answer 30

No

Question 31

Can chloroquine prevent relapses of P. vivax and P. ovale?

Answer 31

No

Question 32

What other conditions can chloroquine treat?

Answer 32

-Extraintestinal amebiasis -rheumatoid arthritis (RA) -discoid lupus erythematosus

Question 33

Name four side effects of chloroquine.

Answer 33

-Retinopathy -hemolysis (G6PD deficiency) -muscle weakness -exacerbation of psoriasis

Question 34

How long does hydroxychloroquine stay in the body?

Answer 34

Over a month

Question 35

What is its prophylactic dosing schedule of hydroxychloroquine?

Answer 35

Once weekly

Question 36

Against which malaria species is amodiaquine highly suppressive?

Answer 36

P. vivax and P. falciparum

Question 37

What side effects are associated with amodiaquine?

Answer 37

Hepatitis and agranulocytosis

Question 38

Has curative activity against P. falciparum

Answer 38

Amodiaquine

Question 39

What is mefloquine effective against?

Answer 39

Multi-drug resistant P. falciparum

Question 40

Who should avoid mefloquine?

Answer 40

Patients with depression, anxiety, psychosis, or major psychiatric disorders

Question 41

All can cause hemolytic anemia in G6PD deficient patients

Answer 41

8-AMINOQUINOLINES

Question 42

Effective only against the exoerythrocytic stages of malaria

Answer 42

PRIMAQUINE

Question 43

What makes primaquine unique?

Answer 43

Only agent for radical cure of P. vivax and P. ovale malarias

Question 44

gametocidal for all four plasmodia species, transmission of the disease can be prevented * not used as prophylaxis * MOA: disrupt the parasites mitochondria

Answer 44

PRIMAQUINE

Question 45

primarily used in the treatment of **Giardiasis** but is also effective against tapeworm and malaria, and topically against leishmaniasis

Answer 45

QUINACRINE

Question 46

Can quinacrine be used with primaquine?

Answer 46

No, due to increased toxicity

Question 47

Enumerate all polycyclic antimalarial drugs

Answer 47

-Doxycycline -Halofantrine -Artemisinin

Question 48

What is doxycycline's MOA?

Answer 48

Inhibits protein synthesis by reversibly inhibiting the 30S ribosomal subunit

Question 49

What is Doxycycline's use in malaria?

Answer 49

Prophylaxis for chloroquine and sulfadoxine-pyrimethamine resistant P. falciparum

Question 50

What is halofantrine classified as?

Answer 50

A schizonticide

Question 51

From what is artemisinin derived?

Answer 51

Dry leaves of Artemisia annua (sweet wormwood)

Question 52

It interferes with the parasites ability to synthesize folic acid

Answer 52

Sulfadoxine

Question 53

It inhibits the reduction of folic acid to its active tetrahydrofolate coenzyme form

Answer 53

Pyrimethamine

Question 54

Indicated for Prophylaxis and treatment of chloroquine-resistant P. falciparum and is **active against all the asexual erythrocytic forms**

Answer 54

Sulfadoxine & Pyrimethamine

Question 55

metabolized to cycloguanil

Answer 55

Proguanil

Question 56

combination is against both erythrocytic and exoerythrocytic Plasmodium

Answer 56

Atovaquone & Proguanil

Question 57

indicated for malaria resistant to chloroquine, halofantrine, mefloquine and amodiaquine

Answer 57

Atovaquone & Proguanil

Question 58

* these two interfere with heme metabolism, thereby stopping development of the parasite in the erythrocyte states

Answer 58

Artemether + Lumefantrine